Note: Descriptions are shown in the official language in which they were submitted.
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SKIN CARE MOISTURIZING AND SUNSCREEN COMPOSITIONS COMPRISING ORGANIC
PARTICULATE MATERIAL
Field of the Invention
The present invention relates to topical compositions with an aqueous
continuous phase
suitable for providing high levels of moisturisation within a product which
has highly
acceptable skin feel properties. More particularly, the invention relates to
topical
compositions which, in addition to moisturisation, also provide protection
against the
harmful effects of ultraviolet radiation, while maintaining optimum skin feel.
The
compositions of the present invention are especially useful for the treatment
of the skin on
the face and hands and also on other areas of the body.
Bacli~round
It has long been a feature of many types of topical compositions, including
skin care
compositions, that they comprise ingredients with moisturisation, skin
regulating and IJV
protection benefits. Such compositions are used to both improve the skin
hydration levels
and to protect the skin from the harmful and damaging effects of ultraviolet
radiation. In
today's environments, when consumers are increasingly exposed to very skin
drying
conditions, such as air conditioned buildings, and where UV radiation is
becoming more
harmful as a result of the depletion of the ozone layer, there is an growing
desire for skin
care products, especially facial products, which protect against, and repair
the damaged
from, these harmful daily assaults.
Conversely, such skin benefit agents, especially organic sunscreens and water
soluble
humectants and vitamins, can be highly tacky in their skin feel with the
result that
compositions containing significant levels of these ingredients have highly
undesirable skin
feel properties including excessive greasiness, stickiness and application
drag. In addition,
when these high levels of humectants are combined with thickeners the
tackiness can be
exacerbated. Thus, until now, there has been a trade off between formulating
topical
compositions with efficacious levels of said benefit imparting ingredients
whilst
simultaneously minimising the levels of these same ingredients so that the
final product has
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acceptable skin feel properties for the consumer. Net, to date, in order to
achieve
acceptable skin feel properties, topical compositions have tended to comprise
sub-optimal
levels of the efficacious, high tack ingredients resulting in multiple
applications over an
extended period being required to achieve desired skin benefits. Since
ingredients with the
worst tack properties are often water soluble this problem is exacerbated in
topical
compositions with an aqueous continuous phase. This is because the ingredients
with the
highly tacky properties, when present or solubilised within the aqueous phase,
come into
high levels of contact with the skin upon application. It is therefore
desirable to provide a
topical composition with an aqueous continuous phase which comprises
efficacious levels
of ingredients with skin benefits, particularly moisturisation and UV
protection benefits,
whilst at the same time having consumer acceptable skin feel properties.
To date the inclusion of particulate materials, including both organic and
inorganic
particles, have been reported in skin care compositions to affect the texture
of both the
skin and the composition itself. See, for example, 'Quantification of the Soft-
Focus
Effect', Cosmetics & Toiletries, Vol. 111, July 1996, pp. 57-61, which
discloses that skin
lines can be physically filled with reflective substances such as Ti02. US-A-
4,892,726,
issued to Toshiba Silicone Co. Ltd, describes the use of
polymethylsilsesquioxane powders
in makeup and cosmetic compositions which are smooth upon application and
impart
natural colour. These particles are now available, in a variety of particle
size grades, from
Toshiba Silicone Co. Ltd under the name Tospearl~. WO 00/24372 describes
topical
compositions comprising 0.5% to 25% of a particulate material having a
refractive index
from 1.35 to 1.6 and a particle size from 2~m to 30~,m, in conjunction with
other
appearance improving actives such as vitamin B3 compounds and retinoids, for
imparting
visual improvement to the skin. The particles disclosed therein similarly
include
Tospearl~ 145A which has a median particle size of about 4.Sp,m. Similarly,
copending
application PCT/LTS99/04748 discloses topical compositions comprising 0.1% to
10%
organic particulate material, again with a refractive index from 1.3 to 1.7,
which are
suitable for imparting an essentially immediate improvement in skin feel and
appearance.
EP-A-692,242 discloses the use of hollow, deformable particles of a size of
from 1 to 250
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p,m, most preferably 18 ~m for reducing the sticky feel of essentially
anhydrous
compositions which are rich in fatty substances; EP-A-908,175 discloses stable
cosmetic
compositions comprising at least one fatty phase, cross linked elastomeric
organopolysiloxanes and high levels of organosiloxane particles; and EP-A-
790,055
discloses the use of partially cross linked elastomeric organosiloxane
polymers, in
combination with a fatty phase and preferably enclosed within a fatty phase,
for preparing
compositions which provide a matt appearance to the skin. These applications
disclose a
variety of cosmetic compositions with improved skin feel and which
additionally have
improved skin appearance properties. However, the applications do not disclose
aqueous
compositions with highly efficacious levels of moisturisation and UV
protection benefit
agents.
The compositions and disclosures of the prior art provide useful advances in
the art of
cosmetic skin treatment and the use of organic particulates in conjunction
with skin benefit
agents. However, they do not adequately teach how to provide both efficacious
levels of
skin moisturisation and UV protection ingredients in an aqueous based topical
composition
which additionally has consumer acceptable skin feel properties.
Surprisingly it has now been found that the high tack negatives of topical
skin care
compositions with an aqueous continuous phase, which also contain highly
efficacious
levels of moisturisation and UV protection ingredients, can be reduced by
additionally
comprising one or more types of organic particulate, with a defined particle
size and
critical surface tension, within the composition. Importantly, the
improvements of the skin
feel properties are so considerable that high levels of moisturisation in
conjunction with
organically derived UV protection, can be achieved within a formulation.
Previously such
combinations would not have been possible due to the unacceptable tackiness.
Additionally it has also been found that if the organic particulate is pre-
mixed in a low
viscosity organosiloxane oil the improvement in skin feel achieved is even
greater.
Without wishing to be bound by theory it is believed that inclusion of the
particulate
materials contributes to minimising friction on product application. Upon
product
application the particles locate themselves at the product residue/air
interface, sitting proud
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of the product residue surface. Thus the contact of the skin with the product
residue is
minimised and the skin feel is improved. In order to ensure that the
particulates are
delivered in the most efficient way to the skin surface during application it
is preferred that
the particulate is premixed in a carrier oil. The particulates are completely
wetted out by
the carrier oil and the low viscosity, and therefore the high mobility, of the
pre-mix ensures
that the particles are efficiently spread over the skin surface on product
application.
It is an object of the present invention to provide topical compositions with
an aqueous
continuous phase suitable for imparting high levels of moisturisation and UV
protection to
the skin. It is another object of the present invention to provide topical
compositions
containing a particulate material eg polymethylsilsesquioxane, which ofd sets
the tackiness
of the formulations to deliver desirable skin feel properties. It is another
object of the
present invention to provide compositions which are useful for delivering
desired levels of
moisturisation and UV protection without the need for multiple applications.
These, and other objects of this invention, will become apparent in light of
the following
disclosure.
Summary of the Invention
The present invention relates to topical cosmetic composition with an aqueous
continuous
phase, in the form of a lotion, cream or gel, comprising:
i) from 0.01% to 25%, by weight, of an organic particulate material
having a median particle size of from 0. S to 30 ~,m;
ii) greater than 8%, by weight, of a humectant selected from glycerine,
polyalkylene glycol, urea, D or DL panthenol, hexane-1, 2, 6- triol,
guanidine or its derivatives, alkylene glycols such as butylene glycol
and propylene glycol, and mixtures thereof;
iii) from 2% to 20%, by weight, organic sunscreen.
The compositions are useful for imparting highly ei~icacious levels of
moisturisation and
UV protection whilst maintaining acceptable skin feel properties.
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This invention further relates to manufacturing methods for enhancing the skin
feel benefits
and cosmetic methods of delivering the moisturisation and UV protections
benefits by
topical application of the subject compositions.
Detailed Description of the Invention
All percentages and ratios used herein are by weight of the total composition
and all
measurements made are at 25°C, unless otherwise designated. Unless
otherwise indicated
all percentages, ratios and levels of ingredients referred to herein are based
on the actual
amount of the ingredient, and do not include solvent, fillers or other
materials which may
be combined with the ingredient in commercially available products.
All publications cited herein are hereby incorporated by reference in their
entirety, unless
otherwise indicated.
The term "dermatologically-acceptable," as used herein, means that the
compositions, or
components thereof, are suitable for use in contact with human skin without
undue
toxicity, incompatibility, instability, allergic response, and the like.
The term "safe and effective amount" as used herein means an amount of a
compound,
component, or composition sui~icient to significantly induce a positive
benefit, preferably a
positive skin appearance or feel benefit, including independently the benefits
disclosed
herein, but low enough to avoid serious side erects, i.e. to provide a
reasonable benefit to
risk ratio, within the scope of sound medical judgement.
Active and other ingredients useful herein may be categorised or described
herein by their
cosmetic and/or therapeutic benefit or their postulated mode of action.
However, it is to
be understood that the active and other ingredients useful herein can in some
instances
provide more than one cosmetic and/or therapeutic benefit or operate via more
than one
mode of action. Therefore, classifications herein are made for the sake of
convenience and
are not intended to limit an ingredient to the particularly stated application
or applications
listed.
The elements of these compositions are described in more detail below.
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WO 01/89466 PCT/USO1/15596
Essential Elements of the Composition
Organic Particulate Material
The composition comprises from about 0.01% to about 25%, preferably from about
0.1%
to about 15%, more preferably from about 0.2% to about 5%, of organic
particulate. It is
highly preferred that the organic particulate has a median particle size of
from about 0.5 to
about 30 ~.m, preferably from about 0.5 to about 15~,m, more preferably from
about 0.7 to
about 10 ~m and even more preferably from about 1 to about 7.S~,m. The median
particle
size is refers to the particulate material in the neat form i.e. in the
essentially pure, powder
form. Particular methods of measuring particle size may, however, require the
particulate
material to be dispersed in an inert carrier, such as a pure oil, in order to
measure the
particle size distribution. Median particle size can be determined by any
suitable method
known in the art, such as by using coulter-counter equipment or the ASTM
Designation
E20 - 85 "Standard Practice for Particle Size Analysis of Particulate
Substances in the
Range of 0.2 to 75 Micrometers by Optical Microscopy", ASTM Volume 14.02,
1993. It
is preferred that more than 50%, preferably more than 60%, more preferably
more than
70% of particles fall within the size ranges prescribed for the respective
median values.
Preferred particles are free-flowing, solid materials. By solid it is meant
that the particles
are preferably non elastomeric and non deformable. Particles are selected from
organosilicone polymers, polyethylene, polyacrylonitrile, polyacrylic acid or
derivatives
thereof, polymethacrylic acid, polystyrene, polytetrafluoroethylene (PTFE),
poly(vinylidene chloride), polyamide and mixtures thereof. More preferably
organic
particulate material is selected from organosilicone polymers and mixtures
thereof, and
even more preferably is polymethylsilsesquioxane. Copolymers derived from
monomers of
the afore-mentioned materials can also be used. Suitable commercially
available examples
of the polymethylsilsesquioxane organic particulate material are Tospearl~ 145
which has
a median particle size of about 4.5 ~m and Tospearl~ 1320 which has a median
particle
size of 12~m. A further representative commercially available example is
Fluoropure
100C from Shamrock Inc, which is a polytetrafluoroethylene organic particulate
material.
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Another representative commercially available example is EA-209~ from Kobo
which is
an ethylene / acrylic acid copolymer having a median particle size of about 10
~,m.
The organic particulate material preferably has a critical surface tension of
less than
SOmN/m, preferably less than 40mN/m and more preferably less than 35mN/m. The
critical surface tension is taken to mean that as defined by Drew and Myers in
"Surfaces,
Interfaces and Colloids, Principles and Applications" 1991 Ch 17, pp 364-369,
(VCH
Publishers Inc, New York) and is measured, in the absence of doubt, by contact
angle
measurements of a series of related liquids with different surface tensions as
also outlined
in the aforementioned reference.
Humectants
Compositions of the present invention comprise from about 8% to about 30%,
preferably
from about 8.5% to about 20% and more preferably from about 9% to about 15%,
by
weight, humectant. Preferred humectants include, but are not limited to,
compounds
selected from glycerine, polyoxyalkylene glycol, urea, D or DL panthenol,
hexane - l, 2, 6,
- triol, guanidine or its derivatives, alkylene glycols such as butylene
glycol or propylene
glycol. Highly preferred humectants are glycerine, urea and mixtures thereof.
The above
listed compounds may be incorporated singly or in combination. The
aforementioned
compounds may give rise to high tack levels, especially when used at the
preferred levels
of greater than 8%. It has been found, however, that this tacky feel can be
effectively
offset by using the humectants in combination with the organic particulates,
as described
by the present invention.
Organic ~S'unscreens
Compositions of the present invention comprise an organic sunscreen. Suitable
sunscreens
can have UVA absorbing properties, UVB absorbing properties or a mixture
thereof. The
exact amount of the sunscreen active will vary depending upon the desired Sun
Protection
Factor, ie the "SPF" of the composition as well as the desired level of UVA
protection.
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WO 01/89466 PCT/USO1/15596
The compositions of the present invention preferably comprise an SPF of at
least 10,
preferably at least 15. (SPF is a commonly used measure of photoprotection of
a
sunscreen against erythema. The SPF is defined as a ratio of the ultraviolet
energy
required to produce minimal erythema on protected skin to that required to
products the
same minimal erythema on unprotected skin in the same individual. See Federal
Register,
43, No 166, pp. 38206-38269, August 25, 1978). Compositions of the present
invention
comprise from about 2% to about 20%, more typically from about 4% to about
14%, by
weight, of organic sunscreen. Suitable sunscreens include, but are not limited
to, those
found in the CTFA I~tef national Cosmetic Ihg~°edieht Dictionary and
Handbook, 7'h
edition, volume 2 pp. 1672, edited by Wenninger arid McEwen (The Cos»aetic,
Toiletry,
aid Pragrayace Association, I~c., Washington, D. G, 1997).
The compositions of the present invention preferably comprise a UVA absorbing
sunscreen actives which absorb UV radiation having a wavelength of from about
320nm to
about 400nm. Suitable UVA absorbing sunscreen actives are selected from
dibenzoylmethane derivatives, anthranilate derivatives such as
methylanthranilate and
homomethyl, 1-N-acetylanthranilate, and mixtures thereof. Examples of
dibenzoylmethane
sunscreen actives are described in US Patent No 4,387,089 issued to Depolo;
and in
Sunscreens: Development, Evaluation, and Regulatory Aspects edited by N. J.
Lowe alid
N. A. Shaath, Marcel Dekker, Inc (1990). The UVA absorbing sunscreen active is
preferably present in an amount to provide broad spectrum UVA protection
either
independently, or in combination with, other UV protective actives which may
be present
in the composition.
Preferred UVA sunscreen actives are dibenzoylmethane sunscreen actives and
their
derivatives. They include, but are not limited to, those selected from 2-
methyldibenzoylmethane, 4-methyldibenzoylmethane, 4-isopropyldibenzoylmethane,
4-
tert-butyldibenzoylmethane, 2, 4-dimethyldibenzoylmethane, 2, 5-
dimethyldibenzoylmethane, 4, 4'-diisopropylbenzoylmethane, 4-(l, 1-
dimethylethyl)-4'-
methoxydibenzoylmethane, 2-methyl-5-isopropyl-4'-methoxydibenzoylmethane, 2-
methyl-
5-tert-butyl-4'-methoxy-dibenzoylmethane, 2, 4-dimethyl-4'-
methoxydibenzoylmethane, 2,
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6-dimethyl-4'-tert-butyl-4'methoxydibenzoylmethane, and mixtures thereof.
Preferred
dibenzoyl sunscreen actives include those selected from 4-(l, 1-dimethylethyl)-
4'-
methoxydibenzoylmethane, 4-isopropyldibenzoylmethane, and mixtures thereof. A
more
preferred sunscreen active is 4-(l, 1-dimethylethyl)-4'-
methoxydibenzoylmethane.
The sunscreen active 4-(1, 1-dimethylethyl)-4'-methoxydibenzoylmethane, which
is also
known as butyl methoxydibenzoylmethane or Avobenzone, is commercially
available under
the names of Parsol~ 1789 from Givaudan Roure (International) S. A. (Basel,
Switzerland) and Eusolex~ 9020 from Merck & Co., Inc (Whitehouse Station, NJ).
The
sunscreen 4-isoproplydibenzoylmethane, which is also known as
isopropyldibenzoylmethane, is commercially available from Merck under the name
of
Eusolex~ 8020.
The compositions of the present invention preferably further comprise a UVB
sunscreen
active which absorbs W radiation having a wavelength of from about 290nm to
abut
320nm. The compositions comprise an amount of the UVB sunscreen active which
is safe
and effective to provide UVB protection either independently, or in
combination with,
other UV protective actives which may be present in the compositions. The
compositions
preferably comprise from about 0.1% to abut 16%, more preferably from about
0.1% to
about 12%, and most preferably from about 0.5% to about 8% by weight, of UVB
absorbing organic sunscreen.
A wide variety of UVB sunscreen actives are suitable fox use herein.
Nonlimiting
examples of such organic sunscreen actives are described in US Patent No
5,087,372
issued February 11, 1992 to Iiaffey et al.; and US Patent Nas 5,073,371 and
5,073,372
both issued on December 17, 1991 to Turner et al.. Preferred UVB sunscreen
actives are
selected from 2-ethylhexyl-2-cyano-3, 3-diphenylacrylate (referred to as
octocrylene), 2-
phenyl-benzimidazole-5-sulphonic acid (PBSA), cinnamates and their derivatives
such as
2-ethylhexyl-p-methoxycinnamate and octyl-p-methoxycinnamate, TEA salicylate,
octyldimethyl PABA, camphor derivatives and their derivatives, and mixtures
thereof.
Preferred organic sunscreen actives are 2-ethylhexyl-2-cyano-3, 3-
diphenylacrylate
(referred to as octocrylene), 2-phenyl-benzimidazole-5-sulphonic acid (PBSA),
octyl-p-
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methoxycinnamate, and mixtures thereof. Salt and acid neutralised forms of the
acidic
sunscreens are also useful herein. When organic sunscreen salts, such as PBSA,
are used
within compositions of the present invention they can disrupt the action of
the thickener
with the result that the final product may have sub optimal rheology. This can
be
countered by the addition of higher levels of thickener, fatty alcohols or
nonionic
surfactants such that the rheology of the final product returns to the desired
level.
An agent may also be added to any of the compositions useful in the present
invention to
stabilise the UVA sunscreen to prevent it from photo-degrading on exposure to
UV
radiation and thereby maintaining its UVA protection efficacy. A wide range of
compounds have been cited as providing these stabilising properties and should
be chosen
to compliment both the UVA sunscreen and the composition as a whole. Suitable
stabilising agents include, but are not limited to, those described in US
Patents Nos
5,972,316; 5,968,485; 5,935,556; 5,827,508 and Patent WO 00/06110. Preferred
examples of stabilising agents for use in the present invention include 2-
ethylhexyl-2-
cyano-3, 3-diphenylacrylate (referred to as octocrylene), ethyl-2-cyano-3, 3-
diphenylacrylate, 2-ethylhexyl-3, 3-diphenylacrylate, ethyl-3, 3-bis(4-
methoxyphenyl)acrylate, and mixtures thereof. 2-ethylhexyl-2-cyano-3, 3-
diphenylacrylate
is most preferred.
An agent may also be added to any of the compositions useful in the present
invention to
improve the skin substantivity of those compositions, particularly to enhance
their
resistance to being washed oil by water, or rubbed oil A preferred agent which
will
provide this benefit is a copolymer of ethylene and acrylic acid. Compositions
comprising
this copolymer are disclosed in U.S. Patent 4,663,157, Brock, issued May 5,
1987.
Balahce of the Composition
The compositions described herein are aqueous, preferably oil in water
emulsions, and can
contain a variety of other optional components suitable for rendering such
compositions
more cosmetically, aesthetically, or otherwise, acceptable or to provide
the~tn with
additional usage benefits, provided that such optional components are
physically and
CA 02408700 2002-11-13
WO 01/89466 PCT/USO1/15596
chemically compatible with the essential components, and method of
preparation,
described herein and do not unduly impair stability, efftcacy or other use
benefits
associated with the compositions of the present invention. Optional components
may be
dispersed, dissolved or the like in the carrier of the present compositions.
Such conventional optional ingredients are well known to those skilled in the
art. These
include, but are not limited to, emollients, oil absorbents, antimicrobial
agents, binders,
buffering agents, denaturants, cosmetic astringents, external analgesics, film
formers,
humectants, opacifying agents, perfumes, pigments, skin soothing and healing
agents,
preservatives, propellants, skin penetration enhancers, solvents, suspending
agents,
emulsifiers, cleansing agents, thickening agents, solubilising agents, waxes,
inorganic
sunblocks, sunless tanning agents, antioxidants and/or radical scavengers,
chelating agents,
anti-acne agents, anti-inflammatory agents, desquamation agents/exfoliants,
organic
hydroxy acids, vitamins, natural extracts and inorganic paxticulates such as
silica and boron
nitride. Nonexclusive examples of such materials are described in Harry's
Cosmeticolog_y,
7th Ed., Harry & Wilkinson (Hill Publishers, London 1982); in Pharmaceutical
Dosage
Forms- Disperse S.stems; Lieberman, Rieger & Banker, Vols. 1 (1988) & 2
(1989);
Marcel Decker, Inc.; in The Chemistry and Manufacture of Cosmetics, 2nd. Ed.,
deNavarre (Van Nostrand 1962-1965); and in The Handbook of Cosmetic Science
and
Technolo~v, 1st Ed.. Knowlton & Pearce (Elsevier 1993) can also be used in the
present
invention.
Preferred compositions have an apparent viscosity of from about 5,000 to about
200,000
mPa.s (centipoise). For example, preferred lotions have an apparent viscosity
of from
about 10,000 to about 40,000 mPa.s; preferred creams have an apparent
viscosity of from
about 30,000 to about 160,000 mPa.s. Apparent viscosity can be determined
using a
Brookfield DVII RV viscometer, spindle TD, at Srpm, or the equivalent thereof.
The
viscosity is determined on the composition after the composition has been
allowed to
stabilise following its preparation, generally at least 24 hours under
conditions of 25°C and
ambient pressure after preparation of the composition. Apparent viscosity is
measured
with the composition at a temperature of 25°C, after 30 seconds spindle
rotation.
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The compositions of the present invention are usually formulated to have a pH
of 9.5 or
below and in general have a pH in the range from about 4.5 to about 9, more
preferably
from about 5 to about 8.5. Some compositions, particularly those comprising an
additional active such as salicylic acid, require a lower pH in order for the
additional active
to be fully efficacious. These compositions are usually formulated to have a
pH of from
about 2.5 to about 5, more preferably from about 2.7 to about 4.
Ca~t~ier
The compositions of the present invention preferably comprise a safe and
effective amount
of a dermatologically acceptable carrier, suitable for topical application to
the skin within
which the essential materials and optional other materials are incorporated to
enable the
essential materials and optional components to be delivered to the skin at an
appropriate
concentration. The carrier can thus act as a diluent, dispersant, solvent, or
the like for any
active ingredients which ensures that they can be applied to, and distributed
evenly over,
the selected target at an appropriate concentration.
Compositions of the present invention comprise an aqueous continuous phase and
preferably comprise an oil in water emulsion in which a hydrophobic phase,
e.g., a lipid, oil
or oily material, is dispersed within the aqueous phase. In emulsion
technology, the term
"dispersed phase" is a term well-known to one skilled in the art which means
that the phase
exists as small particles or droplets that are suspended in and surrounded by
a continuous
phase. The dispersed phase is also known as the internal or discontinuous
phase. Oil-in-
water emulsions typically comprise from about 1 % to about 50% (preferably
about 1 % to
about 30%) ~ of the dispersed hydrophobic phase and from about 1% to about 99%
(preferably from about 40% to about 90%) of the continuous hydrophilic phase.
The
emulsion may also comprise a gel network, such as described in G. M.
Eccleston,
Application of Emulsion Stability Theories to Mobile and Semisolid O/W
Emulsions,
Cosmetics & Toiletries, Vol. 101, November 1996, pp. 73-92, incorporated
herein by
reference.
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Highly preferred carriers are liquid or semi-solid, such as creams, lotions
and gels.
Preferably the carrier is in the form of a lotion, cream or a gel, with
sufficient thickness, or
yield point, to prevent the particles from sedimenting. The carrier can itself
be inert or it
can possess dermatological benefits of its own. The carrier should also be
physically and
chemically compatible with the essential components described herein, and
should not
unduly impair stability, efficacy or other use benefits associated with the
compositions of
the present invention.
The type of carrier utilised in the present invention depends on the types of
product form
desired for the composition. The topical compositions useful in the subject
invention may
be made into a wide variety of product forms such as are known in the art.
These include
but are not limited to, lotions, creams, gels, sticks, sprays, ointments,
pastes and mousses.
These product forms may comprise several types of carriers including, but not
limited to,
solutions, aerosols, emulsions, gels, solids and liposomes.
Preferred carriers contain a dermatologically acceptable, hydrophilic diluent.
Suitable
hydrophilic diluents include water, organic hydrophilic diluents such as C 1 -
C4
monohydric alcohols and low molecular weight glycols and polyols, including
propylene
glycol, polyethylene glycol (e.g. of MW 200-600), poly-propylene glycol (e.g.
of MW
425-2025), glycerol, butylene glycol, butane-l, 2, 4- triol, sorbitol esters,
hexane-l, 2, 6-
triol, ethanol, iso-propanol, ethoxylated ethers, propoxylated ethers and
combinations
thereof. The diluent is preferably liquid. Water is an especially preferred
diluent. The
composition preferably comprises at least about 60% of the hydrophilic
diluent.
Emollients
The topical compositions of the subject invention generally comprise from
about 1% to
about 50%, preferably from about 1.5% to about 15% of a dermatologically
acceptable
emollient. Emollients tend to lubricate the skin, increase the smoothness and
suppleness of
the skin, prevent or relieve dryness of the skin, and/or protect the skin.
Emollients axe
typically water-immiscible, oily or waxy materials and emollients with high
molecular
13
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WO 01/89466 PCT/USO1/15596
weights can confer tacky properties to a topical composition. A wide variety
of suitable
emollients are known and may be used herein. Sagarin, Cosmetics~Science and
Technolo~y, 2nd Edition, Vol. 1, pp. 32-43 (1972), contains numerous examples
of
materials suitable as an emollient. AlI emollients discussed in application WO
00/24372
should be considered as suitable for use in the present invention although
preferred
examples are outlined in further detail below:
i) Straight and branched chain hydrocarbons having from about 7 to about 40
carbon
atoms, such as dodecane, squalane, cholesterol, hydrogenated polyisobutylene,
isohexadecane and the C7-C40 isoparai~ns, which are C7-C40 branched
hydrocarbons.
ii) Cl-C30 alcohol esters of CI-C3p carboxylic acids and of C2-C30
dicarboxylic acids,
e.g. , isononyl isononanoate, isopropyl myristate, myristyl propionate,
isopropyl
stearate, isopropyl isostearate, methyl isostearate, behenyl behenate, dioctyl
maleate,
diisopropyl adipate, and diisopropyl dilinoleate.
iii) C1-C30 mono- and poly- esters of sugars and related materials. These
esters are
derived from a sugar or polyol moiety and one or more carboxylic acid
moieties.
Depending on the constituent acid and sugar, these esters can be in either
liquid or
solid form at room temperature. . Examples include: glucose tetraoleate, the
galactose
tetraesters of oleic acid, the sorbitol tetraoleate, sucrose tetraoleate,
sucrose
pentaoleate, sucrose hexaoleate, sucrose heptaoleate, sucrose octaoleate,
sorbitol
hexaester in which the carboxylic acid ester moieties are palmitoleate and
arachidate
in a 1:2 molar ratio, and the octaester of sucrose wherein the esterifying
carboxylic
acid moieties are laurate, linoleate and behenate in a 1:3:4 molar ratio.
Other
materials include cottonseed oil or soybean oil fatty acid esters of sucrose.
Other
examples of such materials are described in WO 96/16636, incorporated by
reference
herein. A particularly preferred material is known by the INCI name sucrose
polycottonseedate
14
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WO 01/89466 PCT/USO1/15596
iv) Vegetable oils and hydrogenated vegetable oils. Examples of vegetable oils
anal
hydrogenated vegetable oils include safflower oil, castor oil, coconut oil,
cottonseed
oil, menhaden oil, palm kernel oil, palm oil, peanut oil, soybean oil,
rapeseed oil,
linseed oil, rice bran oil, pine oil, sesame oil, sunflower seed oil,
partially and fully
hydrogenated oils from the foregoing sources, and mixtures thereof.
EmulsifierslSurfactants
Compositions herein preferably contain an emulsifier and/or surfactant,
generally to help
disperse and suspend the discontinuous phase within the continuous aqueous
phase. A
surfactant may also be useful if the product is intended for skin cleansing.
For convenience
hereinafter emulsifiers will be referred to under the term 'surfactants', thus
'surfactant(s)'
will be used to refer to surface active agents whether used as emulsifiers or
for other
surfactant purposes such as skin cleansing. Known or conventional surfactants
can be
used in the composition, provided that the selected agent is chemically and
physically
compatible with essential components of the composition, and provides the
desired
characteristics. Suitable surfactants include non-silicone derived materials,
and mixtures
thereof. All surfactants discussed in application WO 00/24372 should be
considered as
suitable for use in the present invention.
The compositions of the present invention preferably comprise from about 0.05%
to about
15% of a surfactant or mixture of surfactants. The exact surfactant or
surfactant mixture
chosen will depend upon the pH of the composition and the other components
present.
Preferred surfactants are nonionic. Among the nonionic surfactants that are
useful herein
are those that can be broadly defined as condensation products of long chain
alcohols, e.g.
Cg-30 alcohols, with sugar or starch polymers ie glycosides. Other useful
nonionic
surfactants include the condensation products of alkylene oxides with fatty
acids (i.e.
alkylene oxide esters of fatty acids). These materials have the general
formula
RCO(X)nOH wherein R is a C10-30 ~kyl group, X is -OCH2CH2- (i.e. derived from
ethylene glycol or oxide) or -OCH2CHCH3- (i.e. derived from propylene glycol
or oxide),
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and n is an integer from about 6 to about 200. Other nonionic surfactants are
the
condensation products of alkylene oxides with 2 moles of fatty acids (i.e.
alkylene oxide
diesters of fatty acids). These materials have the general formula RCO(X)nOOCR
wherein R is a C10-30 ~kYl group, X is -OCH2CH2-(i.e. derived from ethylene
glycol or
oxide) or -OCH2CHCH3-(i.e. derived from propylene glycol or oxide), and n is
an integer
from about 6 to about 100. Even further suitable examples include a mixture of
cetearyl
alcohols, cetearyl glucosides such as those available under the trade name
Montanov 68
from Seppic and Emulgade PL68/50 from Cognis UK Ltd.. An example of a suitable
cetearyl glucoside material without added fatty alcohols is Tego (RTM) Care
CG90
commercially available from Goldschmidt GmbH.
The hydrophilic surfactants useful herein can alternatively or additionally
include any of a
wide variety of cationic, anionic, zwitterionic, and amphoteric surfactants
such as are
known in the art. See, e.g., McCutcheon's, Detergents and Emulsifiers, North
American
Edition (1986), published by Allured Publishing Corporation; U.S. Patent No.
5,011,681
to Ciotti et al., issued April 30, 1991; U.S. Patent No. 4,421,769 to Dixon et
al., issued
December 20, 1983; and U.S. Patent No. 3,755,560 to Dickert et al., issued
August 28,
1973. A wide variety of anionic surfactants are also useful herein. See, e.g.,
U.S. Patent
No. 3,929,678, to Laughlin et al., issued December 30, 1975.
A wide variety of anionic surfactants are also useful herein. See, e.g., U.S.
Patent No.
3,929,678, to Laughlin et al., issued December 30, 1975. Exemplary anionic
surfactants
include the alkoyl isethionates (e.g., C12 - C30), alkyl and alkyl ether
sulfates and salts
thereof, alkyl and alkyl ether phosphates and salts thereof, alkyl methyl
taurates (e.g., C12
- C30), and soaps (e.g., alkali metal salts, e.g., sodium or potassium salts)
of fatty acids.
Amphoteric and zwitterionic surfactants are also useful herein. Examples of
amphoteric
and zwitterionic surfactants which can be used in the compositions of the
present
invention are those which are broadly described as derivatives of aliphatic
secondary and
tertiary amines in which the aliphatic radical can be straight or branched
chain and wherein
one of the aliphatic substituents contains from about 8 to about 22 carbon
atoms
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(preferably Cg - C1g) and one contains an anionic water solubilising group,
e.g., carboxy,
sulfonate, sulfate, phosphate, or phosphonate. Examples are alkyl imino
acetates, and
iminodialkanoates and aminoalkanoates, imidazolinium and ammonium derivatives.
Other
suitable amphoteric and zwitterionic surfactants are those selected from the
group
consisting of betaines, sultaines, hydroxysultaines, and branched and
unbranched alkanoyl
sarcosinates, and mixtures thereof.
Thickening Agent (including thickeners and gelling agents)
The compositions of the present invention can also preferably comprise a
thickening agent,
more preferably from about 0.1% to about 5%, even more preferably from about
0.1% to
about 3%, and most preferably from about 0.25% to about 2%, of a thickening
agent.
Preferred compositions of the present invention include a thickening agent
selected from
carboxylic acid polymers, crosslinked polyacrylates, polyacrylamides, xanthan
gum and
mixtures thereof, more preferably selected polyacrylamide polymers, xanthan
gum and
mixtures thereof. Preferred polyacrylamides are predispersed in a water-
immiscible
solvent such as mineral oil and the like, containing a surfactant (HLB from
about 7 to
about 10) which helps to facilitate water dispersibility of the
polyacrylamide. Most
preferred for use herein is the non-ionic polymer under the CTFA designation:
polyacrylamide and isoparaf~n and laureth-7, available under the trade name
Sepigel 305
from Seppic Corporation. Also useful are acrylic acid/ethyl acrylate
copolymers and the
carboxyvinyl polymers sold by the B.F. Goodrich Company under the trade mark
of
Carbopol resins. Suitable Carbopol resins are described in W098/22085. All
thickening
agents discussed in application WO 00/24372 should be considered as suitable
for use in
the present invention.
Inorganic Sunscreens
In addition to the organic sunscreens compositions of the present invention
can
additionally comprise inorganic physical sunblocks. Nonlimiting examples of
suitable
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WO 01/89466 PCT/USO1/15596
physical sunblocks are described in CTFA International Cosmetic Ingredient
Dictionary,
6a' Edition, 1995, pp. 1026-28 and 1103, Sayre, R. M. et al., "Physical
Sunscreens", J.
Soc. Cosmet. Chem., vol 41, no 2, pp. 103-109 (1990). Preferred inorganic
physical
sunblocks are zinc oxide and titanium dioxide, and mixtures thereof.
When used, the physical sunblocks are present in an amount such that the
present
compositions are transparent on the skin (ie non-whitening), preferably less
than or equal
to about 5%. When titanium dioxide is used, it can have an anatase, rutile, or
amorphous
structure. Physical sunblock particles, eg titanium dioxide and zinc oxide,
can be uncoated
or coated with a variety of materials including but not limited to amino
acids, aluminium
compounds such as alumina, aluminium stearate, aluminium Iaurate, and the
like;
carboxylic acids and their salts eg stearic acid and its salts; phospholipids
such as lecithin;
organic silicone compounds; inorganic silicone compounds such as silica and
silicates; and
mixtures thereof. A preferred titanium dioxide is commercially available from
Tayca
(Japan) and is distributed by Tri-K Industries (Emerson, NJ) under the MT
micro-ionised
series (eg MT 100SAS).
The compositions of the present invention preferably comprise from about 0.1%
to about
10%, more preferably from about 0.1% to about 4%, and most preferably from
about
0.5% to about 2.5%, by weight, of inorganic sunscreen.
Actives for regulating skin condition
The compositions of the invention optionally comprise a safe and effective
aanount of an
active for regulating skin condition including prophylactically and
therapeutically
regulating the skin condition. Prophylactically regulating skin condition
includes delaying,
minimising, and / or preventing visible and / or tactile discontinuities in
the skin.
Therapeutically regulating the skin condiments includes ameliorating eg
diminishing,
minimising, and / or effacing such discontinuities. Regulating the skin
condition also
involves improving the skin appearance and / or feel. Also included is
regulating the signs
of ageing which can involve prophylactically regulating and / or
therapeutically regulating
one or more of such signs eg fine Iines, wrinkles, pores etc.
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WO 01/89466 PCT/USO1/15596
Ingredients that are known to be useful for regulating the skin condition are
selected from
Vitamin B3 compounds, retinoids, and combinations thereof. As described for
the
humectants, the aforementioned compounds may, when used by themselves, give
rise to a
high level of tack, especially when used at the higher levels. It has been
found, however,
that this tacky feel can be offset by using the particulates of the present
invention. The
compositions of the present invention preferably comprise from about 0.1% to
about 15%,
more preferably from about 0.3% to about 10%, even more preferably from about
1 to
about 5% of the active.
As used herein, "vitamin B3 compound" means a compound having the formula:
-R
wherein R is - CONH2 (i. e., niacinamide), - COON (i. e., nicotinic acid) or -
CH20H (i. e.,
nicotinyl alcohol); derivatives thereof; and salts of any of the foregoing.
One or more
vitamin B3 compounds, or their salts, or mixtures thereof may be used herein.
In a
preferred embodiment, the vitamin B3 compound typically contains less than
about 50% of
the compound in a salt form. As used herein, "retinoid" includes all natural
and/or
synthetic analogues of Vitamin A or retinol-like compounds which possess the
biological
activity of Vitamin A in the skin as well as the geometric isomers and
stereoisomers of
these compounds. Again, all skin regulating materials discussed in application
WO
00/24372 should be considered as suitable for use in the present invention.
Anti-Inf Zammato~y Agents
A safe and effective amount of an anti-inflammatory agent may be added to the
compositions of the subject invention, preferably from about 0.1% to about 5%,
more
preferably from about 0.1 % to about 2%, of the composition. The anti-
inflammatory
agent enhances the skin appearance benefits of the present invention, e.g.,
such agents
contribute to a more uniform and acceptable skin tone or colour. The exact
amount of
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WO 01/89466 PCT/USO1/15596
anti-inflammatory agent to be used in the compositions will depend on the
particular anti-
inflammatory agent utilised since such agents vary widely in potency.
Anti-inflammatory agents useful herein include steroids such as
hydrocortisone; non-
steroidal anti-inflammatory drugs (NSAa?S) such as ibuprofen; panthenol and
ether and
ester derivatives thereof e.g. panthenol ethyl ether, panthenyl triacetate;
pantothenic acid
and salt and ester derivatives thereof, especially calcium pantothenate; aloe
vera, bisabolol,
allantoin and compounds of the liquorice (the plant genus/species Glycyrrhiza
1~ abra)
family, including glycyrrhetic acid, glycyrrhizic acid, and derivatives
thereof e.g. salts such
as ammonium glycyrrhizinate and esters such as stearyl glycyrrhetinate.
Particularly
preferred herein are panthenol, pantothenic acid and their ether, ester or
salt derivatives
and mixtures thereof; suitable levels are from about 0.1 to about 5%,
preferably from
about 0.5 to about 3%. Panthenol is especially preferred.
Ahti-0xidantslRadical Scavenges
Compositions of the subject invention can further include an anti-
oxidant/radical
scavenger. The anti-oxidant/radical scavenger is especially useful for
providing protection
against UV radiation which can cause increased scaling or texture changes in
the stratum
corneum and against other environmental agents which canmcause skin damage.
Suitable
amounts are from about 0.1% to about 10%, more preferably from about 1% to
about 5%,
of the composition.
Anti-OxidantslRadical ~S'cavengers
Anti-oxidants/radical scavengers such as ascorbic acid (vitamin C) and its
salts, ascorbyl
esters of fatty acids, ascorbic acid derivatives (e.g., magnesium ascorbyl
phosphate), (3-
carotene, tocopherol (vitamin E), tocopherol sorbate, tocopherol acetate,
other esters of
tocopherol, butylated hydroxy benzoic acids and their salts, gallic acid and
its alkyl esters,
especially propyl gallate, uric acid and its salts and alkyl esters, sorbic
acid and its salts,
amines (e.g., N,N-diethylhydroxylamine, amino-guanidine), sulfhydryl compounds
(e.g.,
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glutathione), dihydroxy fumaric acid and its salts, bioflavonoids, lysine,
methionine,
proline, superoxide dismutase, silymarin, tea extracts, grape skin/seed
extracts, melanin,
and rosemary extracts may be used. Preferred anti-oxidants/radical scavengers
are
selected from tocopherol acetate, tocopherol sorbate and other esters of
tocopherol, more
preferably tocopherol acetate. As described for the humectants, the
aforementioned
compounds may, when used by themselves, give rise to a high level of tack,
especially
when used at the higher levels. It has been found, however, that this tacky
feel can be
oiTset by using the particulates of the present invention.
Chelato~s
The inclusion of a chelating agent is especially useful for providing
protection against UV
radiation which can contribute to excessive scaling or skin texture changes
and against
other environmental agents which can cause skin damage. A suitable amount is
from
about 0.01% to about 1%, more preferably from about 0.05% to about 0.5%, of
the
composition. Exemplary chelators that are useful herein are disclosed in U.S.
Patent No.
5,487,884, incorporated herein by reference. Preferred chelators useful in
compositions of
the subject invention are ethylenediamine tetraacetic acid (EDTA),
furildioxime, and
derivatives thereof.
Desquamatiou AgentslExfoliants
A safe and effective amount of a desquamation agent may be added to the
compositions of
the subject invention, more preferably from about 0.1% to about 10%, even more
preferably from about 0.2% to about 5%, ,also preferably from about 0.5% to
about 4% of
the composition. Desquamation agents enhance the skin appearance benefits of
the
present invention. For example, the desquamation agents tend to improve the
texture of
the skin (e.g., smoothness). A variety of desquamation agents are known in the
art and are
suitable for use herein, including organic hydroxy acids such as salicylic
acid, glycolic acid,
lactic acid, 5-octanoyl salicylic acid, hydroxyoctanoic acid, hydroxycaprylic
acid, and
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WO 01/89466 PCT/USO1/15596
lanolin fatty acids. One desquamation system that is suitable for use herein
comprises
sulphydryl compounds and zwitterionic surfactants and is described in WO
96/01101,
incorporated herein by reference. Another desquamation system that is suitable
for use
herein comprises salicylic acid and zwitterionic surfactants and is described
in
WO 95/13048, incorporated herein by reference. Salicylic acid is preferred.
Skin Lightening Agents
The compositions of the present invention can also comprise a skin lightening
agent.
When used, the compositions preferably comprise from about 0.1% to about 10%,
more
preferably from about 0.2% to about 5%, also preferably from about 0.5% to
about 2%, of
a skin lightening agent. Suitable skin lightening agents include those known
in the art,
including kojic acid, arbutin, ascorbic acid and derivatives thereof, e.g.,
magnesium
ascorbyl phosphate. Further skin lightening agents suitable for use herein
also include
those described in WO 95/34280 and WO 95/23780; each incorporated herein by
reference.
Silicohe Based Ingredients
The compositions of the present invention preferably also contain silicone
based
ingredients. Preferred examples are discussed below:
i) Silicone Based Emollients. Organopolysiloxane oils may be used as
ingredients with
emollient benefits in the present compositions. Suitable organopolysiloxane
oils
include volatile, non-volatile, or a mixture of volatile and non-volatile
silicones. The
term "non-volatile" as used in this context refers to those silicones that are
liquid
under ambient conditions and have a flash point (under one atmospheric of
pressure)
of or greater than about 100°C. The term "volatile" as used in this
context refers to
those silicone oils having a flash point of less than 100°C. Suitable
organopolysiloxanes can be selected from a wide variety of silicones spanning
a broad
range of volatilities and viscosities. Non-volatile polysiloxanes are
preferred.
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WO 01/89466 PCT/USO1/15596
Suitable silicones are disclosed in U.S. Patent No. 5,069,897, issued December
3,
1991, which is incorporated by reference herein in its entirety. Preferred for
use
herein are organopolysiloxanes selected from the group consisting of
polyalkylsiloxanes, alkyl substituted dimethicones, dimethiconols,
polyalkylaryl
siloxanes, and mixtures thereof. More preferred for use herein are
polyalkylsiloxanes
and cyclomethicones. Preferred among the polyalkylsiloxanes are dimethicones
for
example DC200 available from Dow Corning and SF96 available from GE Silicone.
ii) Silicone Based Emulsifiers. Preferred emulsions of the present invention
include a
silicone containing emulsifier or surfactant. A wide variety of silicone
emulsifiers are
useful herein. These silicone emulsifiers are typically organically modified
organopolysiloxanes, also known to those skilled in the art as silicone
surfactants.
Useful silicone emulsifiers include dimethicone copolyols. These materials are
polydimethyl siloxanes which have been modified to include polyether side
chains
such as polyethylene oxide chains, polypropylene oxide chains, mixtures of
these
chains, and polyether chains containing moieties derived from both ethylene
oxide and
propylene oxide. Other examples include alkyl-modified dimethicone copolyols,
i.e.,
compounds which contain CZ-C30 pendant side chains. Still other useful
dimethicone
copolyols include materials having various cationic, anionic, amphoteric, and
zwitterionic pendant moieties.
Preparation of Compositions
The present invention relates to cosmetic compositions with an aqueous
continuous phase
comprising organic particulate, greater than 8% humectant and organic
sunscreen.
Compositions are preferably an oil in water emulsion. These can be prepared
according to
procedures usually used in cosmetics and that are well known and understood by
those
skilled in the art with materials of similar phase partitioning can be added
in any order.
Preferably the organic particulate is slowly and homogeneously premixed into a
carrier oil
prior to addition to the balance of the composition. This results in the
organic particulate
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WO 01/89466 PCT/USO1/15596
being able to more e~ciently of set the negative tack properties of the skin
benefit agents
than if the particulate is added directly to the composition. Once formed the
premix
should be preferably added immediately to the balance of the composition to
maintain the
benefits. If the balance of the composition is an emulsion then it is
preferable to prepare
the emulsion prior to addition of the premix. This avoids disruption of the
premix that
could potentially occur as a result of the high shear step during
emulsification.
Premix Composition
The premix preferably comprises from about 5% to about 90%, preferably from
about
20% to about 80% and more preferably from about 40% to about 75%, by weight,
of
organic particulate. Preferably it has a viscosity of less than SOOOmPa.s,
preferably less
than 2000mPa.s which is measured using an airbearing Haake rheostress RS75
rheometer
using a C35/2Ti cone and plate and 0.105mm gap distance. The viscosity is
measured at
31°C (skin temperature) at a shear rate of 20s 1. Additionally it is
preferred that the premix
forms, and remains stable within, a discrete phase within the balance of the
composition
such that it can be viewed as distinct droplets, with a diameter of greater
than 0.1 wm,
when viewed at a magnification of 40x using a standard light microscope.
However, it is
recognised that, dependent upon the other ingredients within the composition,
there may
be migration from one phase to another of several of the other ingredients
once the
composition is formed which may prevent the maintenance of the pre-mix as a
truly
discrete phase.
Carrier Oil
It is preferred that the carrier oil has a surface tension of less than that
of the chosen
organic particulate and a viscosity of less than about 350mPa.s, preferably
less than about
100mPa.s and more preferably less than about 75mPa.s The viscosity of the
carrier oil is
also measured at 31°C (skin temperature), in the same way as already
described for the
total premix.
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WO 01/89466 PCT/USO1/15596
The carrier oil preferably is a organosilicone based oil selected from non
volatile and
volatile organosiloxanes, and mixtures thereof. The term "non-volatile" as
used in this
context refers to those silicones that are liquid under ambient conditions and
have a flash
point (under one atmospheric of pressure) of or greater than about
100°C. The term
"volatile" as used in this context refers to those silicone oils having a
flash point of less
than 100°C. Suitable organopolysiloxanes can be selected from a wide
variety of silicones
spanning a broad range of volatilities and viscosities. Non-volatile
organopolysiloxanes
are preferred. Suitable silicone caxrier oils axe disclosed in U.S. Patent No.
5,069,897,
issued December 3, 1991. Preferred for use herein are organopolysiloxanes
selected from
the group consisting of polyalkylsiloxanes, alkyl substituted dimethicones,
dimethiconols,
polyalkylaryl siloxanes, and mixtures thereof. More preferred for use herein
are
polyalkylsiloxanes and cyclomethicones. Preferred among the polyalkylsiloxanes
are
dimethicones, for example DC200 available from Dow Corning and SF96, available
from
GE Silicone.
Examples
The following examples further illustrate the preferred embodiments within the
scope of
the present invention. These examples are given solely for the purpose of
illustration and
are not to be construed as limitations of the present invention as many
variations of the
invention are possible without departing from its spirit or scope. Unless
otherwise
indicated, all ingredients are expressed as a weight percentage of the active
ingredient.
Phase I
EXAMPLE I II DI IV V VI
Parsol HS 1 1.00 1.00 1.00 - - 1.00
Parso117891 1.00 1.50 2.00 2.00 2.00 1.00
Octocrylene2 1.00 2.00 1.50 1.00
Octyl salicylate3 2.50 3.50 4.50 3.00 2.50
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WO 01/89466 PCT/USO1/15596
Parsol MCXI - - - - 5.00 -
Stearyl Alcohol 0.40 0.40 0.48 0.80 1.2 0.40
Cetyl Alcohol 1.00 0.80 0.72 I.80 0.80 1.00
Hydrofol Acid 0.10 0.10 0.10 0.10 0.10 0.10
Myrj 594 0.10 0.10 0.10 0.10 0.10 0.10
IsopropylIsostearates 0.75 1.00 1.00 0.5 2.00 0.75
SEFA Cottonate6 1.50 1.00 1.80 - - 1.50
Ethyl paraben 0.15 0.15 0.20 0.20 0.25 0.15
Propyl paraben 0.20 0.20 0.30 0.25 0.25 0.20
Tocopherol acetate 0.25 0.50 0.75 0.50 - 0.25
Isohexadecane - 4.00 - 0.50 1.00 -
Petrolatum - - - 1.20 0.50 -
Phase II
EXAMPLE I II III IV V VI
Deionised Water to to to to to to
100 100 100 100 100 100
Glycerine 9.00 12.00 - 15.00 - 9.00
Kobo GWL75CAP7 0.30 0.25 0.50 0.50 0.50 0.30
Polyethylene glycol 20081.00 - - 10.00 1.00
Hexane-126-triol - 0.50 3.00 - - -
Urea - - 10.00 - - -
Montanov 68 9 - 0.50 0.20 0.50 0.20 -
Emulgade PL681501 - - - - - 0.25
Di-sodium EDTA 0.10 0.10 0.10 0.10 0.10 0.10
~ ~
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WO 01/89466 PCT/USO1/15596
Phase TIZI
EXAMPLE T II III IV V VI
Fluoropure 100C11 0.50 - - - - -
Tospear1145A12 - 1.00 - - 1.00 1.00
Tospear1120A12 - - - 1.00 - -
Orgasol 2002 EXD N COS ' - 1.00 - - -
13
DC200 Scsl4 - 0.65 1.50 - - -
DC200 50cs14 0.17 - - 0:50 - -
DC200100cs14 - - - 2.50 - -
Isohexadecane 0.15 - 0.50 - - -
Additional Ingredients
EXAMPLE I II 11I IV V VI
Sepige13059 1.50 2.00 3.00 2.00 3.00 1.50
Sodium Hydroxide pellets 0.013 0.013 0.013 0.013 0.013 0.013
Benzyl alcohol 0.20 0.25 0.25 0.25 0.30 0.20
D-Panthenol - 0.50 0.50 - 1.00 -
Niacinamide - 3.00 - 2.00 5.00 -
DC Q2-140314 1.60 2.00 1.50 2.00 2.50 1.60
Dry F1o15 _ _ _ _ _ 2
1. Supplied by Hoffmann-LA Roche, Inc., 340 Kingsland Street, Nutley, NJ 07110-
1199
2. Supplied by BASF Aktiengesellschaft, MEM/KU - D 205, 67056 Ludwigshafen,
Gexmany
3. Supplied by Haarmann & Reimer Corporation, 70 Diamond Road, P. O. Boy 175,
Springfield, NJ
07081-0175
27
CA 02408700 2002-11-13
WO 01/89466 PCT/USO1/15596
4. PEG 100 Stearate supplied by ICI, PO Box 90, Wilton Centre, Middlesborough,
Cleveland, England.
TS6 8JE
5. Supplied by Scher Chemicals Inc, Industrial West, Clifton, NJ 07012
6. A Cl-C30 monoester or polyester ~of sugars and one or more carboxylic acid
moieties as described
herein, preferably a sucrose polyester in which the degree of esterification
is 7-8, and in which the fatty
acid moieties are C18 mono- and/or di-unsaturated and behenic, in a molar
ratio of unsaturates:behenic
of 1:7 to 3:5, more preferably the octaester of sucrose in which there are
about 7 behenic fatty acid
moieties and about 1 oleic acid moiety in the molecule, e.g., sucrose ester of
cottonseed oil fatty acids.
7. Supplied by Kobo Products Inc, 690 Montrose Ave, So Plainfield, NJ 07080
8. Supplied by Union Carbide Corporation, Danbury, Conn., USA
9. Supplied by Seppic, 75 Quai D'Orsay, Paris
10. Supplied by Cognis UK Ltd., 3rd floor, Eleanor House, 33!35 Eleanor Cross
Road, Waltham Cross,
EN8 7LE, UK
11. Supplied by Shamrock Technologies Inc., Newark, NJ07114, USA
12. Supplied by GE Silicones, Plasticslaan 1/P0 Box 117, 4600 AC Bergen op
Zoom, Netherlands
13. Supplied by Elf Atochem, 4, cours Michelet, La Defense 10, Cedex 42,
92091, Paris
14. Supplied by Dow Corning, Kings Court, 185 Kinds Rd, Reading, Berks, RGl
4EX
15. Aluminium Starch Octenyl Succinate supplied by National Starch and
Chemical Limited, Braunston,
Daventry, Northants., NNll 7KL, UK
Phase I was prepared by mixing the oil soluble emulsifiers, emollients and oil
soluble
preservatives with gentle heating until an homogenous mixture was formed.
Phase II was prepared by heating water, glycerine, Kobo titanium dioxide,
urea,
polyethylene glycol, hexane-l, 2, 6-trio! in a vessel to about 80°C
while mixing with a
Heidolph pitch blade turbine mixer at 200rpms, cooling to 75°C a.nd
adding Montanov 68
or Emulgade PL68/50 and disodium EDTA. (Note that the Montanov 68 and Emulgade
PL68/50 can be added into the oil phase instead of the water phase if
desired). Stirring
was continued for a further 5 minutes prior to addition of Phase I. The
mixture of Phase I
with Phase II was homogenised using an Ultraturax T25 (IKA - Labortechnik) at
13500rpms for about 10 minutes and then cooled to 65°C.
If required the particulate of Phase III was stirred into the carrier oil at
room temperature
with an impeller stirrer at 50-150rpms. Once an homogenous mixture was formed
it was
28
CA 02408700 2002-11-13
WO 01/89466 PCT/USO1/15596
added immediately to the Phase I / Phase II emulsion. If no carrier oil was
present in
Phase III the particulate was added slowly, with stirring, to the Phase I /
Phase II
emulsion.
The resultant mixture was cooled further and once it reached 60°C the
Sepigel 305 and
NaOH were added. The remainder of the ingredients were added after the mixture
had
been further cooled to 50°C. The resultant product was cooled further
prior to packaging.
29
